Acetomycin (1) is a polyfunctionalized lactone that has demonstrated potent antitumor activity in cell culture assays against a variety of tumors including those in a human cloning system. The in vivo antitumor activity, however, is greatly diminished owing to a rapid deacetylation and degradation of the compound. Herein is proposed a study in which prodrugs of 1 and certain congeners of 1 will be synthesized and evaluated for antitumor activity. A total synthesis of acetomycin is proposed. Evaluation of all new compounds will be conducted in both in vitro and in vivo screens.